Relative Bioavailability of Single Oral Doses of 150 mg Dabigatran Etexilate With or Without Oral Administration of Verapamil in Two Different Dosages (240 mg and 480 mg Daily) (Open-label, Fixed-sequence Design), and Relative Bioavailability of Single Oral Doses of 150 mg Dabigatran Etexilate Given With or Without Single Oral Doses of 120 mg (IR) or 240 mg (ER) of Verapamil Administered at Different Time Points Relative to Dabigatran Etexilate Dosing in Healthy Male and Female Volunteers (Open-label, Randomised, Five-way Crossover Design, Phase I Study)

简要总结

主要结局

次要结局

• Cmax (maximum measured concentration of free dabigatran)(up to 107 hours)
• AUC0-infinity (area under the concentration-time curve of free dabigatran over the time interval from 0 extrapolated to infinity)(up to 107 hours)
• t1/2 (terminal half-life of the analyte in plasma)(up to 107 hours)
• Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular dose)(up to 107 hours)
• tmin,ss (time from last dosing to the minimum concentration of verapamil at steady state over a uniform dosing interval τ)(up to 107 hours)
• Cpre,ss (predose concentration of verapamil at steady state immediately before administration of the next dose)(up to 107 hours)
• Cavg (Average concentration of verapamil at steady state)(up to 107 hours)
• MRTpo,ss (mean residence time of verapamil in the body at steady state after oral administration)(up to 107 hours)
• Vz/F,ss (apparent volume of distribution during the terminal phase λz at steady state following an extravascular administration)(up to 107 hours)
• Ae0-24 (amount of dabigatran that is eliminated in urine from the time interval 0-24h)(up to 107 hours)
• fe0-24 (fraction of administered drug excreted unchanged in urine from time point 0- 24h)(up to 107 hours)
• CLR0-24 (renal clearance of dabigatran from the time point 0 until the time point 24h )(up to 107 hours)
• AUEC0-24 (area under the effect curve)(up to 107 hours)
• ERmax (maximum effect ratio)(up to 107 hours)
• Occurence of Adverse Events(within 5 days after last drug administration)
• AUC0-infinity (area under the concentration-time curve of verapamil over the time interval from 0 extrapolated to infinity)(up to 107 hours)
• Cmax (maximum measured concentration of verapamil)(up to 107 hours)
• tmax (time from dosing to the maximum concentration of the analyte in plasma)(up to 107 hours)
• λz (terminal rate constant in plasma)(up to 107 hours)
• AUC0-tz (area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the time of the last quantifiable data point)(up to 107 hours)
• AUC0-24 (area under the concentration-time curve of the analyte in plasma over the time interval from 0 to 24 h after the administration)(up to 107 hours)
• MRTpo (mean residence time of the analyte in the body after oral administration)(up to 107 hours)
• CL/F (apparent clearance of the analyte in the plasma after extravascular administration)(up to 107 hours)
• AUC0-tz,ss (area under the concentration-time curve of verapamil from the time point 0 after the last dose at steady state to the last quantifiable analyte plasma concentration within the uniform dosing interval τ)(up to 107 hours)
• Cmax,ss (maximum concentration of verapamil at steady state)(up to 107 hours)
• tz,ss (time of last measureable concentration of verapamil within the dosing interval τ at steady state)(up to 107 hours)
• tmax,ss (time from last dosing to the maximum concentration of verapamil at steady state on day 4)(up to 107 hours)
• CL/F,ss (apparent clearance of verapamil at steady state after extravascular multiple dose administration)(up to 107 hours)
• Cmin,ss (minimum measured concentration of verapamil at steady state over a uniform dosing interval τ)(up to 107 hours)
• AUCτ,ss (area under the concentration-time curve of verapamil within the uniform dosing interval τ)(up to 107 hours)
• Assessment of Tolerability by investigator(within 5 days after last drug administration)